摘要:
Through the use of the novel receptor NER in a screening procedure, TOFA (5-tetradecyloxy)-2-furan-carboxylic acid) has been found to modulate other receptors and to be a potent potentiator of other drugs. TOFA activates the NER receptor. The NER receptor is a novel member of the steroid hormone receptor family and has been prepared by cDNA cloning from a human osteosarcoma SAOS-2/B10 cell library. Also disclosed is the complete sequence of human NER cDNA; a COS stable expression system; the expressed NER protein; and an assay using the COS expression system. In addition, the invention relates to a method for identifying functional ligands of the NER receptor.
摘要:
The NER receptor is a novel member of the steroid hormone receptor superfamily and has been prepared by cDNA cloning from a human osteosarcoma SAOS-2/B10 cell library. The complete sequence of human NER complementary DNA (Seq. ID No. 1), expression systems including a COS stable expression system, the expressed protein (SEQ. ID No. 2) and an assay using the COS expression system are disclosed. The assay may be used to identify agents which activate transcription mediated by the NER receptor, and which are useful for potentiating the activity of a modulator of a G-protein coupled receptor wherein the G-protein coupled receptor is a member of the steroid hormone receptor superfamily.
摘要翻译:NER受体是类固醇激素受体超家族的新成员,并通过人骨肉瘤SAOS-2 / B10细胞库的cDNA克隆制备。 公开了人NER互补DNA(Seq.ID No.1)的完整序列,包括COS稳定表达系统的表达系统,表达的蛋白质(SEQ ID NO:2)和使用COS表达系统的测定法。 该测定可用于鉴定激活由NER受体介导的转录的试剂,其可用于增强G蛋白偶联受体调节剂的活性,其中G蛋白偶联受体是类固醇激素受体的成员 超家族
摘要:
A novel human protein tyrosine phosphatase (PTP) has been identified and its cDNA has been isolated. This novel PTP, denoted PTP-OB, has a receptor-like three dimensional structure and is present in osteoblasts. PTP-OB is involved in osteoblast differentiation, and modulators of PTP-OB activity in turn modulate osteoblast differentiation, osteoclast differentiation and osteoclast activity.
摘要:
A novel member of the Wnt-family of growth factors, termed Wnt-x, has been identified and DNA encoding the growth factor has been isolated, purified, sequenced and expressed in host cells. This DNA encoding the novel Wnt-x protein and host cells expressing the Wnt-x protein are used to identify modulators of the Wnt-x growth factor.
摘要:
A novel human protein tyrosine phosphatase (PTP) has been identified and its cDNA has been isolated. This novel PTP, denoted PTP-OB, has a receptor-like three dimensional structure and is present in osteoblasts. PTP-OB is involved in osteoblast differentiation, and modulators of PTP-OB activity in turn modulate osteoblast differentiation, osteoclast differentiation and osteoclast activity.
摘要:
A human protein tyrosine phosphatase (PTP) has been identified and its cDNA has been isolated. This PTP, denoted PTP-OB, has a receptor-like three dimensional structure and is present in osteoblasts. PTP-OB is involved in osteoblast differentiation, and modulators of PTP-OB activity in turn modulate osteoblast differentiation, osteoclast differentiation and osteoclast activity.
摘要:
Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, arthritis and joint repair, alone or in combination with other active agents. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.
摘要:
The Macaca mulatta (rhesus monkey) Nur77 (rhNur77) nuclear receptor and the nucleic acid encoding the rhNur77 nuclear receptor are described. Further described are methods for identifying analytes that modulate expression or activity of the rhNur77 nuclear receptor. Analytes that affect Nur77 expression or activity may be used to treat or inhibit inflammatory diseases, for example, osteoarthritis and various bone, neurological, and prostrate disorders. The rhNur77 may also be used to treat various cancers, for example, prostate, ovarian, colon, lung, and gastric cancer.
摘要:
The Macaca mulatta (rhesus monkey) Nur77 (rhNur77) nuclear receptor and the nucleic acid encoding the rhNur77 nuclear receptor are described. Further described are methods for identifying analytes that modulate expression or activity of the rhNur77 nuclear receptor. Analytes that affect Nur77 expression or activity may be used to treat or inhibit inflammatory diseases, for example, osteoarthritis and various bone, neurological, and prostrate disorders. The rhNur77 may also be used to treat various cancers, for example, prostate, ovarian, colon, lung, and gastric cancer.